HUP0400267A2 - Pyrazolo[3,4-d]pyrimidines as therapeutic agents - Google Patents

Pyrazolo[3,4-d]pyrimidines as therapeutic agents

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Publication number
HUP0400267A2
HUP0400267A2 HU0400267A HUP0400267A HUP0400267A2 HU P0400267 A2 HUP0400267 A2 HU P0400267A2 HU 0400267 A HU0400267 A HU 0400267A HU P0400267 A HUP0400267 A HU P0400267A HU P0400267 A2 HUP0400267 A2 HU P0400267A2
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Hungary
Prior art keywords
cra
alkyl
heteroaryl
aryl
nitrogen
Prior art date
Application number
HU0400267A
Other languages
Hungarian (hu)
Inventor
Lee D. Arnold
David Calderwood
Michael M. Friedman
Gavin C. Hirst
Paul Rafferty
Kurt Ritter
Neil Wishart
Original Assignee
Abbott Gmbh & Co. Kg
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Abbott Gmbh & Co. Kg filed Critical Abbott Gmbh & Co. Kg
Publication of HUP0400267A2 publication Critical patent/HUP0400267A2/en

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

A találmány az (I) általános képletű vegyületekre, racém-diasztereomerkeverékeikre, optikai izomerjeikre, gyógyászatilag elfogadható sóikra,p-rodrugjaikra vagy biológiailag aktív metabolitjaikra vonatkozik,ahol a képletben a helyettesítők jellemző jelentése: G jelentése (A)általános képletű csoport, ahol Z100 jelentése (B) általános képletűcsoport vagy egy R1 helyettesítővel szubsztituált alkil-, cikloalkil-,pirrolidinil-, vagy biciklusos aromás nitrogéntartalmú heterociklus;Z110 és Z111 jelentése kovalens kötés vagy adott esetben szubsztituáltszénhidrogéncsoport; Ra és R1 jelentése többek között hidrogénatom, -C(O)O-aril, -C(O)O-heteroaril, -C(O)-a1kil, -C(O)-aril, -C(O)-heteroaril; szubsztituált vagy szubsztituálatlan cikloalkil-,heteroaril-, heteroarilalkoxi-, arilalkoxi-, alkil-S(O)p-, alkil-S-,aril-S(O)p,-, heteroaril-S(O)p- képletű csoport; ahol p értéke 1 vagy2; A jelentése többek között - (1-6 szénatomos szénhidrogéncsoport)-,-O-; -S-; vagy Z110-A-Z111 együtt kovalens kötést alkot; R3 jelentésehidrogénatom, hidroxil-, szubsztituált vagy szubsztituálatlan alkil-,-C(O)-alkil, -C(O)-aril, -C(O)-heteroaril vagy alkoxicsoport; R2jelentése többek között hidrogénatom, tritil-, cikloalkenil-,azaheteroaril- vagy azacikloalkilcsoport, a értéke 1 és D1, G1, J1 ésL1 és Ml jelentése CRa vagy nitrogénatom; vagy a értéke 0 és D1, Gl,L1 és M1 közül az egyik jelentése NRa; Dl, Gl, L1 és M1 egyikénekjelentése CRa és a többi jelentése CRa vagy nitrogénatom; b értéke 1és D2, G2, J2, L2 és M2 jelentése egymástól függetlenül CRa vagynitrogénatom; vagy b értéke 0 és D2 G2, L2 és M2 közül az egyikjelentése NRa; D2, G2, L2 és M2 egyikének jelentése CRa, és a többijelentése CRa vagy nitrogénatom. A találmány szerinti vegyületekalkalmasak egy betegben protein-kinázok gátlására, ezáltal többekközött hiperproliferatív betegségek és angiogenezis befolyásolására. ÓThe invention relates to the compounds of the general formula (I), their racemic-diastereomer mixtures, their optical isomers, their pharmaceutically acceptable salts, prodrugs or biologically active metabolites, where the typical meaning of the substituents in the formula is: G is a group of the general formula (A), where Z100 is (B) a group of the general formula or an alkyl, cycloalkyl, pyrrolidinyl or bicyclic aromatic nitrogen-containing heterocycle substituted with an R1 substituent; Z110 and Z111 are covalent bonds or optionally substituted hydrocarbon groups; R a and R 1 are hydrogen, -C(O)O-aryl, -C(O)O-heteroaryl, -C(O)-alkyl, -C(O)-aryl, -C(O)-heteroaryl; a substituted or unsubstituted cycloalkyl-, heteroaryl-, heteroarylalkyl-, arylalkyl-, alkyl-S(O)p-, alkyl-S-, aryl-S(O)p,-, heteroaryl-S(O)p- group; where p is 1 or 2; A means, among others, - (hydrocarbon group with 1-6 carbon atoms)-,-O-; -S-; or Z110-A-Z111 together form a covalent bond; R3 is a hydrogen atom, hydroxyl, substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-aryl, -C(O)-heteroaryl or alkoxy; R2 is, inter alia, hydrogen, trityl, cycloalkenyl, azaheteroaryl or azacycloalkyl, the value is 1 and D1, G1, J1 and L1 and M1 are CRa or nitrogen; or the value is 0 and one of D1, Gl, L1 and M1 is NRa; one of Dl, Gl, L1 and M1 is CRa and the others are CRa or nitrogen atom; b is 1 and D2, G2, J2, L2 and M2 are independently CRa or nitrogen atom; or b is 0 and D2 is one of G2, L2 and M2 meaning NRa; One of D2, G2, L2, and M2 is CRa, and the others are CRa or nitrogen. The compounds according to the invention are suitable for inhibiting protein kinases in a patient, thereby influencing, among other things, hyperproliferative diseases and angiogenesis. HE

HU0400267A 2001-03-22 2002-03-22 Pyrazolo[3,4-d]pyrimidines as therapeutic agents HUP0400267A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27804701P 2001-03-22 2001-03-22
PCT/US2002/008996 WO2002076986A1 (en) 2001-03-22 2002-03-22 Pyrazolopyrimidines as therapeutic agents

Publications (1)

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HUP0400267A2 true HUP0400267A2 (en) 2004-08-30

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US (1) US7332497B2 (en)
EP (1) EP1379528A4 (en)
JP (1) JP4319412B2 (en)
KR (1) KR20030088114A (en)
CN (1) CN101426792A (en)
BG (1) BG108268A (en)
BR (1) BR0205890A (en)
CA (1) CA2440714C (en)
CO (1) CO5570669A2 (en)
CZ (1) CZ20032837A3 (en)
EC (1) ECSP034773A (en)
HU (1) HUP0400267A2 (en)
IL (1) IL157640A0 (en)
MX (1) MXPA03008560A (en)
NO (1) NO20034177L (en)
PE (1) PE20030047A1 (en)
PL (1) PL363946A1 (en)
SK (1) SK13122003A3 (en)
UY (1) UY27222A1 (en)
WO (1) WO2002076986A1 (en)
ZA (1) ZA200306887B (en)

Families Citing this family (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
WO2002011769A1 (en) * 2000-08-04 2002-02-14 Human Genome Sciences, Inc. Vascular endothelial growth factor 2
US20050232921A1 (en) * 2001-04-13 2005-10-20 Rosen Craig A Vascular endothelial growth factor 2
AU2002252631A1 (en) * 2001-04-13 2002-10-28 Human Genome Sciences, Inc. Vascular endothelial growth factor 2
EP1385864B1 (en) * 2001-04-13 2010-06-09 Human Genome Sciences, Inc. Anti-VEGF-2 antibodies
US20030199525A1 (en) * 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
DE60304718T2 (en) 2002-08-06 2007-04-26 Astrazeneca Ab CONDENSED PYRIDINES AND PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
WO2004100868A2 (en) * 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
US7429596B2 (en) * 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
DE10344223A1 (en) 2003-09-24 2005-04-21 Merck Patent Gmbh New 2-anilino-1,3-benzoxazole derivatives, are inhibitors of kinases, especially tyrosine- or Raf-kinases, useful e.g. for treating solid tumors, angiogenesis, diabetic retinopathy, inflammation or psoriasis
AU2004282219C1 (en) 2003-10-15 2009-12-17 Osi Pharmaceuticals, Inc. Imidazo [1, 5 - a] pyrazine tyrosine kinase inhibitors
CA2553724A1 (en) * 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
RU2379308C2 (en) * 2004-04-02 2010-01-20 Оси Фармасьютикалз, Инк. 6,6-bicyclic ring substituted heterobicyclic proteinkinase inhibitors
EP1753428A4 (en) * 2004-05-14 2010-09-15 Abbott Lab Kinase inhibitors as therapeutic agents
US20080287405A1 (en) * 2004-05-14 2008-11-20 Thannickal Victor J Compositions and Methods Relating to Protein Kinase Inhibitors
AR053090A1 (en) 2004-07-20 2007-04-25 Osi Pharm Inc IMIDAZOTRIAZINS AS PROTEIN KINASE INHIBITORS AND THEIR USE FOR THE PREPARATION OF MEDICINES
WO2006068760A2 (en) * 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
US8575164B2 (en) * 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
PT2004654E (en) * 2006-04-04 2013-08-27 Univ California Pyrazolopyrimidine derivatives for use as kinase antagonists
PL2529621T3 (en) * 2006-09-22 2017-06-30 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
RU2446796C2 (en) * 2006-12-26 2012-04-10 Фармасайкликс, Инк. Method for using histone deacetylase and biomarker monitoring in combined therapy
US20080200458A1 (en) * 2007-01-18 2008-08-21 Joseph Barbosa Methods and compositions for the treatment of body composition disorders
US20080194557A1 (en) * 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
MX2009009304A (en) 2007-03-01 2009-11-18 Novartis Ag Pim kinase inhibitors and methods of their use.
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
JP5347202B2 (en) * 2007-03-28 2013-11-20 ファーマサイクリックス，インク． Breton tyrosine kinase inhibitor
GB2467670B (en) 2007-10-04 2012-08-01 Intellikine Inc Chemical entities and therapeutic uses thereof
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
ES2647163T3 (en) 2008-01-04 2017-12-19 Intellikine, Inc. Purine-substituted isoquinolinone derivatives useful as PI3K inhibitors
US20110046144A1 (en) * 2008-01-18 2011-02-24 Mulvihill Mark J Imidazopyrazinol derivatives for the treatment of cancers
US7998688B2 (en) * 2008-03-07 2011-08-16 OSI Pharmaceuticals, LLC Inhibition of EMT induction in tumor cells by anti-cancer agents
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
EP2252293B1 (en) 2008-03-14 2018-06-27 Intellikine, LLC Kinase inhibitors and methods of use
WO2009143051A1 (en) * 2008-05-19 2009-11-26 Osi Pharmaceuticals, Inc. Substituted imidazopyr-and imidazotri-azines
US20090301928A1 (en) * 2008-06-05 2009-12-10 United Comb & Novelty Corporation Packaging For Lipped Containers
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
KR20110039326A (en) 2008-07-08 2011-04-15 인텔리카인, 인크. Kinase inhibitors and methods of use
CN102159214A (en) 2008-07-16 2011-08-17 药品循环公司 Inhibitors of bruton's tyrosine kinase for treatment of solid tumors
GEP20135849B (en) 2008-09-02 2013-06-10 Novartis Ag Picolinamide derivatives as kinase inhibitors
CA2738429C (en) * 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
JP5819195B2 (en) * 2008-10-16 2015-11-18 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Fusion ring heteroaryl kinase inhibitors
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
BRPI1016245A2 (en) 2009-04-20 2015-09-01 Osi Pharmaceuticals Llc Preparation of c-pyrazine methylamines.
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
EP2427192A1 (en) * 2009-05-07 2012-03-14 OSI Pharmaceuticals, LLC Use of osi-906 for treating adrenocortical carcinoma
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
GEP201706639B (en) 2009-08-17 2017-03-27 Intellikine Llc Heterocyclic compounds and uses thereof
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
US20110130711A1 (en) * 2009-11-19 2011-06-02 Follica, Inc. Hair growth treatment
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
US9765037B2 (en) 2010-01-28 2017-09-19 University Of Washington Through Its Center For Commercialization Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases
WO2011094628A1 (en) * 2010-01-28 2011-08-04 University Of Washington Compositions and methods for treating toxoplasmosis. cryptosporidiosis and other apicomplexan protozoan related diseases
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
CA2800521A1 (en) * 2010-05-24 2011-12-01 Toa Eiyo Ltd. Fused imidazole derivative
AU2011261185A1 (en) 2010-06-03 2013-01-10 Pharmacyclics, Inc. The use of inhibitors of Bruton's tyrosine kinase (Btk)
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
CA2804648C (en) * 2010-07-09 2019-01-22 The Walter And Eliza Hall Institute Of Medical Research Protein kinase inhibitors and methods of treatment
EP2637669A4 (en) 2010-11-10 2014-04-02 Infinity Pharmaceuticals Inc Heterocyclic compounds and uses thereof
CA2824197C (en) 2011-01-10 2020-02-25 Michael Martin Processes for preparing isoquinolinones and solid forms of isoquinolinones
WO2012097196A1 (en) * 2011-01-12 2012-07-19 Acea Biosciences Inc. Pyrazolopyrimidine derivatives and uses as anticancer agents
TWI592411B (en) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 Combination of kinase inhibitors and uses thereof
AU2012255759B2 (en) 2011-05-17 2017-08-10 Principia Biopharma, Inc. Kinase inhibitors
EP2731612A4 (en) 2011-07-13 2015-04-08 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
JP6027611B2 (en) 2011-07-19 2016-11-16 インフィニティー ファーマシューティカルズ， インコーポレイテッド Heterocyclic compounds and uses thereof
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
CA2846431A1 (en) 2011-08-29 2013-03-07 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
JP6342805B2 (en) 2011-09-02 2018-06-13 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Substituted pyrazolo [3,4-D] pyrimidine and uses thereof
CN103917231B (en) 2011-09-13 2016-09-28 药品循环有限责任公司 Combination formulations of histone deacetylase inhibitor and bendamustine and application thereof
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9173883B2 (en) 2012-05-21 2015-11-03 Novartis Ag Ring-substituted N-pyridinyl amides as kinase inhibitors
CA3218491A1 (en) 2012-06-04 2013-12-12 Pharmacyclics Llc Crystalline forms of a bruton's tyrosine kinase inhibitor
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
KR20180088926A (en) 2012-07-24 2018-08-07 파마싸이클릭스 엘엘씨 Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
JP6327713B2 (en) * 2012-07-27 2018-05-23 国立研究開発法人理化学研究所 Acute myeloid leukemia treatment or recurrence inhibitor
CA2882367C (en) 2012-09-10 2021-11-09 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
MX2015003874A (en) 2012-09-26 2015-12-16 Univ California Modulation of ire1.
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
JP2015537033A (en) 2012-11-15 2015-12-24 ファーマサイクリックス，インク． Pyrrolopyrimidine compounds as kinase inhibitors
WO2014122474A1 (en) 2013-02-07 2014-08-14 Takeda Pharmaceutical Company Limited Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
CA2907726A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase
US9518026B2 (en) 2013-05-20 2016-12-13 University Of Washington Through Its Center For Commercialization 5-aminopyrazole-4-carboxamide inhibitors of CDPK1 from T. gondii and C. parvum
MX367554B (en) * 2013-06-05 2019-08-27 C&C Res Lab Heterocyclic derivatives and use thereof.
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
TWI649081B (en) 2013-08-02 2019-02-01 製藥公司 Method for treating solid tumors
WO2015023703A1 (en) 2013-08-12 2015-02-19 Pharmacyclics, Inc. Methods for the treatment of her2 amplified cancer
BR112016006978A2 (en) 2013-09-30 2017-08-01 Pharmacyclics Llc bruton tyrosine kinase inhibitors
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9359365B2 (en) 2013-10-04 2016-06-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
KR102452866B1 (en) 2013-10-25 2022-10-07 파마싸이클릭스 엘엘씨 Methods of treating and preventing graft versus host disease
BR112016018948B1 (en) 2014-02-21 2023-01-17 Principia Biopharma Inc USE OF COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT, SULFONIC ACID OR CARBOXYLIC ACID SALT OF COMPOUND, AMORPHOUS FORM OF PHARMACEUTICALLY ACCEPTABLE SALT OF COMPOUND, PHARMACEUTICAL COMPOSITION AND USE THEREOF
CA2943075C (en) 2014-03-19 2023-02-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
CA2942528A1 (en) 2014-03-20 2015-09-24 Pharmacyclics Inc. Phospholipase c gamma 2 and resistance associated mutations
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
EP3174539A4 (en) 2014-08-01 2017-12-13 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase
CN106573002A (en) 2014-08-07 2017-04-19 药品循环有限责任公司 Novel formulations of a bruton's tyrosine kinase inhibitor
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US10196397B2 (en) 2014-11-19 2019-02-05 Sun Pharmaceutical Industries Limited Process for the preparation of ibrutinib
PL3233103T3 (en) 2014-12-18 2021-04-19 Principia Biopharma Inc. Treatment of pemphigus
CA2972239A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of bruton's tyrosine kinase inhibitor
EP3273966B1 (en) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CN105906630B (en) * 2015-04-06 2018-10-23 四川百利药业有限责任公司 Two substitutional amine-group compounds of N- (1H- pyrazoles -5- bases) pyrimido pyrazoles -4,6- as FGFR inhibitor
GB201508747D0 (en) * 2015-05-21 2015-07-01 Univ Edinburgh Compounds
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP3313839A1 (en) 2015-06-24 2018-05-02 Principia Biopharma Inc. Tyrosine kinase inhibitors
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016321218A1 (en) * 2015-09-09 2018-03-29 Warren C. Lau Methods, compositions, and uses of novel fyn kinase inhibitors
NZ740616A (en) 2015-09-14 2023-05-26 Infinity Pharmaceuticals Inc Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
TW201806953A (en) * 2016-04-26 2018-03-01 印度商托仁特生技有限公司 Substituted fused pyrimidinone compounds
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN107513068A (en) * 2016-06-16 2017-12-26 中国科学院上海药物研究所 A kind of new compound and its preparation and application with FGFR inhibitory activity
MX2018016227A (en) 2016-06-24 2019-07-08 Infinity Pharmaceuticals Inc Combination therapies.
KR102515813B1 (en) 2016-06-29 2023-03-30 프린시피아 바이오파마, 인코퍼레이티드 Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
EP3559002A4 (en) 2016-12-23 2021-02-17 Arvinas Operations, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
CN108503648B (en) * 2018-04-27 2020-04-14 安徽医科大学 Styryl pyrazolopyrimidine compound, pharmaceutical composition, preparation method and application
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
TW202103708A (en) 2019-04-12 2021-02-01 美商里伯賽恩斯有限責任公司 Bicyclic heteroaryl derivatives as ectonucleotide pyrophosphatase phosphodiesterase 1 inhibitors
CN110015985B (en) * 2019-05-16 2022-05-13 河南师范大学 2- (alpha-deuterium-alpha-hydroxy-alpha-aryl/alkyl) aza-aromatic hydrocarbon compound and preparation method and application thereof
WO2021038540A1 (en) 2019-08-31 2021-03-04 Sun Pharma Advanced Research Company Limited Cycloalkylidene carboxylic acids and derivatives as btk inhibitors
AU2020436612A1 (en) 2020-03-16 2022-09-01 Flash Therapeutics, Llc Compounds for treating or inhibiting recurrence of acute myeloid leukemia
BR112022025012A2 (en) 2020-06-08 2023-02-14 Halia Therapeutics Inc NEK7 KINASE INHIBITORS
JP2024513227A (en) 2021-04-05 2024-03-22 ハリア・セラピューティクス・インコーポレイテッド NEK7 inhibitor

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4966849A (en) 1985-09-20 1990-10-30 President And Fellows Of Harvard College CDNA and genes for human angiogenin (angiogenesis factor) and methods of expression
US4966846A (en) * 1987-10-01 1990-10-30 W. R. Grace & Co.-Conn. Molecular cloning and expression of a vibrio proteolyticus neutral protease gene
US5217999A (en) 1987-12-24 1993-06-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Styryl compounds which inhibit EGF receptor protein tyrosine kinase
CA2078214C (en) 1990-04-02 1995-03-28 Robert Lee Dow Benzylphosphonic acid tyrosine kinase inhibitors
US5302606A (en) 1990-04-16 1994-04-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Styryl-substituted pyridyl compounds which inhibit EGF receptor tyrosine kinase
DE69222637T2 (en) 1991-05-10 1998-02-26 Rhone Poulenc Rorer Int UP TO MONO AND BICYCLIC ARYL AND HETEROARYL DERIVATIVES WITH INHIBITING EFFECT ON EGF AND / OR PDGF RECEPTOR TYROSINKINASE
JPH06503095A (en) 1991-05-29 1994-04-07 ファイザー・インコーポレーテッド Tricyclic polyhydroxy tyrosine kinase inhibitor
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
CZ283965B6 (en) 1992-08-06 1998-07-15 Warner-Lambert Company 2-thioindoles, 2-indolinethiones and polysulfides, their selenium analogs and pharmaceutical preparations based thereon
US5330992A (en) 1992-10-23 1994-07-19 Sterling Winthrop Inc. 1-cyclopropyl-4-pyridyl-quinolinones
RO119721B1 (en) 1992-10-28 2005-02-28 Genentech Inc. Antagonists of vascular endotelial cell growth factor
GB9226855D0 (en) 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
AU2103097A (en) 1996-03-15 1997-10-10 Zeneca Limited Cinnoline derivatives and use as medicine
UA54427C2 (en) 1996-05-01 2003-03-17 Елі Ліллі Енд Компані Method for treating eye diseases caused by vascular endotelium growth factor
CN1233177A (en) 1996-05-01 1999-10-27 伊莱利利公司 Therapeutic treatment for VEGF related diseases
GB9707800D0 (en) 1996-05-06 1997-06-04 Zeneca Ltd Chemical compounds
DK1749836T3 (en) 1996-08-23 2009-08-31 Vegenics Ltd Recombinant vascular endothelial cell growth factor D
AU779008C (en) 1999-01-11 2005-06-30 Princeton University High affinity inhibitors for target validation and uses thereof
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
CZ2002936A3 (en) * 1999-09-17 2002-10-16 Abbott Gmbh & Co. Kg Pyrazolopyrimidines functioning as therapeutic preparations

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